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      Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.

      Bioorganic & Medicinal Chemistry Letters

      Weight Gain, metabolism, agonists, Receptors, Cytoplasmic and Nuclear, Rats, pharmacokinetics, chemistry, chemical synthesis, Quinolines, Protein Structure, Tertiary, Naphthalenes, Molecular Conformation, Mice, Ligands, Isoxazoles, Humans, Fluorescence Resonance Energy Transfer, Dogs, Diabetes Mellitus, Experimental, Crystallography, X-Ray, Blood Glucose, Binding Sites, Animals, drug effects

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          Abstract

          To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability parameters relative to 1b. In addition, analog 1c lowered body weight gain and serum glucose in a DIO mouse model of diabetes. Copyright © 2010 Elsevier Ltd. All rights reserved.

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          Journal
          10.1016/j.bmcl.2010.12.089
          21256005

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